GPR17-Targeting Compounds Identified by Omeros Promote Myelination

      GPR17-Targeting Compounds Identified by Omeros Promote Myelination

-Remyelination May Provide a Novel Treatment for Multiple Sclerosis Patients-

PR Newswire

SEATTLE, Nov. 15, 2012

SEATTLE, Nov. 15, 2012 /PRNewswire/ --Omeros Corporation (NASDAQ: OMER) today
announced that GPR17-targeting compounds, which were previously identified by
Omeros in connection with unlocking this orphan receptor, have now been
demonstrated to promote differentiation of the cells that form myelin in the
central nervous system. Myelin is critical for the proper functioning of the
nervous system, and demyelination is associated with multiple nervous system
disorders, including multiple sclerosis (MS), traumatic brain or spinal cord
injury, stroke and Alzheimer's disease. Using its proprietary high-throughput
Cellular Redistribution Assay, Omeros believes that it alone has identified
compounds that interact with GPR17, an orphan G protein-coupled receptor
(GPCR).

"These data are very encouraging," stated Bruce Trapp, Ph.D., founder and
chief scientific officer of Renovo Neural Inc. (RNI), chairman of the
Department of Neurosciences at the Lerner Research Institute, Cleveland
Clinic, and professor of neurosciences at Case Western Reserve University.
"There are no approved remyelinating therapeutics, and the compounds under
development by Omeros could lead to the first oral agents able to stimulate
sufficient remyelination to restore neural function. This would represent a
breakthrough in the treatment of currently irreversible demyelinating
diseases, such as MS and other devastating myelin-related disorders." The
data were generated through Omeros' collaboration with RNI, a company focused
on remyelination research to accelerate drug development for demyelinating
neural diseases.

"GPR17 represents one of Omeros' unlocked GPCRs that we are advancing through
medicinal chemistry," said Gregory A. Demopulos, M.D., chairman and chief
executive officer of Omeros. "The biology of the receptor – its strong link to
remyelination – has been well documented, and Omeros now has identified over
90 compounds that functionally affect its signaling, and many of these are
highly potent. These compounds are drawn from multiple classes of
structurally diverse and tractable small-molecules, enabling the development
of proprietary drugs that could restore function in patients faced with
severely progressive or traumatic demyelinating neural disorders."

Ongoing GPCR Program
Omeros is screening orphan GPCRs against its small-molecule chemical libraries
using its proprietary, high-throughput cellular redistribution assay (CRA).
The CRA detects receptor antagonists, agonists and inverse agonists. Omeros
has announced that it has identified and confirmed sets of compounds that
interact selectively with 46 orphan receptors linked to metastatic melanoma
(GPR19), esophageal squamous cell carcinoma and obesity-related type-2
diabetes (GPR39), hepatocellular carcinoma (GPR80), several types of cancer
(GPR65/TDAG8), squamous cell carcinoma (GPR87), ovarian cancer (GPR150),
pancreatic cancer (GPR182), acute lymphoblastic leukemia (P2Y8/P2RY8), ovarian
and prostate cancer (OGR1), arterial stiffness (GPR25), sleep disorders
(OPN4), cognitive disorders (GPR12), torpor or "suspended animation" and
bipolar disorder (GPR50), anxiety disorders (GPR31), schizophrenia (GPR52,
GPR153), autism (GPR63), bipolar disorder and schizophrenia (GPR78), memory
and inflammatory conditions (GPR83), psychotic and metabolic disorders (GPR27,
GPR85, GPR173), cognition (GPR151), cognitive impairments (MAS1), inflammatory
responses (GPR32), obesity and diabetes (GPR21), appetite control (GPR82,
GPR101), immunological disorders (CCRL2), rheumatoid arthritis and
HIV-mediated enteropathy (GPR15), respiratory and immune disorders (GPR141),
humoral immunity (GPR183), multiple sclerosis (GPR17), osteoarthritis (GPR22),
motor control (GPR139), congenital cataracts and birth defects of the brain
and spinal cord (GPR161), regulation of hematopoietic stem cell
differentiation (GPR171), cancer stem cells and the self-renewal and
maintenance of adult stem cells (LGR4), long-term wound repair, including the
formation of new hair follicles (LGR6) and pain (MRGE). In addition, Omeros
has unlocked GPR20, GPR45, GPR135, GPR162, MRGF and OPN5, which have not yet
been definitively tied to any specific indications but are expressed
preferentially in the gastrointestinal tract (GPR20), brain (GPR45, GPR135 and
GPR162) and eye, brain, testes, spinal cord (OPN5) and dorsal root ganglia
(MRGF).

About G Protein-Coupled Receptors
GPCRs, which mediate key physiological processes in the body, are one of the
most valuable families of drug targets. According to Insight Pharma Reports,
GPCR-targeting drugs represent 30 to 40 percent of marketed pharmaceuticals.
Examples include Claritin® (allergy), Zantac® (ulcers and reflux), OxyContin®
(pain), Lopressor® (high blood pressure), Imitrex® (migraine headache),
Reglan® (nausea) and Abilify® (schizophrenia, bipolar disease and depression)
as well as all other antihistamines, opioids, alpha and beta blockers,
serotonergics and dopaminergics.

The industry focuses its GPCR drug discovery efforts mostly on non-sensory
GPCRs. Of the 363 total non-sensory GPCRs, approximately 240 have known
ligands (molecules that bind the receptors) with nearly half of those targeted
either by marketed drugs (46 GPCRs) or by drugs in development (about 82
GPCRs). There are approximately 120 GPCRs with no known ligands, which are
termed "orphan GPCRs." Without a known ligand, drug development for a given
receptor is extremely difficult.

Omeros uses its proprietary high-throughput CRA to identify small-molecule
agonists and antagonists for orphan GPCRs, unlocking them to drug development.
Omeros believes that it is the first to possess the capability to unlock
orphan GPCRs in high-throughput, and that currently there is no other
comparable technology. Unlocking these receptors could lead to the development
of drugs that act at these new targets. There is a broad range of indications
linked to orphan GPCRs including cardiovascular disease, asthma, diabetes,
pain, obesity, Alzheimer's disease, Parkinson's disease, multiple sclerosis,
schizophrenia, learning and cognitive disorders, autism, osteoporosis,
osteoarthritis and several forms of cancer.

About Omeros Corporation
Omeros is a clinical-stage biopharmaceutical company committed to discovering,
developing and commercializing products targeting inflammation, coagulopathies
and disorders of the central nervous system. The Company's most clinically
advanced product candidates are derived from its proprietary PharmacoSurgery™
platform designed to improve clinical outcomes of patients undergoing a wide
range of surgical and medical procedures. Omeros has four ongoing clinical
development programs. Omeros may also have the near-term capability, through
its GPCR program, to add a large number of new drug targets and their
corresponding compounds to the market. Behind its clinical candidates and GPCR
platform, Omeros is building a diverse pipeline of protein and small-molecule
preclinical programs targeting inflammation, coagulopathies and central
nervous system disorders.

Forward-Looking Statements
This press release contains forward-looking statements as defined within the
Private Securities Litigation Reform Act of 1995, which are subject to the
"safe harbor" created by those sections. These statements include, but are not
limited to, the potential for GPR17-targeting compounds to treat nervous
system disorders, such as MS; that the compounds identified by Omeros could
lead to the development of proprietary drugs; and that Omeros may have
capability, through its GPCR program, to add a large number of new drug
targets and their corresponding compounds to the market. Forward-looking
statements are based on management's beliefs and assumptions and on
information available to management only as of the date of this press release.
Omeros' actual results could differ materially from those anticipated in these
forward-looking statements for many reasons, including, without limitation,
the risks, uncertainties and other factors described under the heading "Risk
Factors" in the Company's Quarterly Report on Form 10-Q filed with the
Securities and Exchange Commission on November 9, 2012. Given these risks,
uncertainties and other factors, you should not place undue reliance on these
forward-looking statements, and the Company assumes no obligation to update
these forward-looking statements publicly, even if new information becomes
available in the future.

SOURCE Omeros Corporation

Contact: Jennifer Cook Williams, Cook Williams Communications, Inc., Investor
and Media Relations, +1-360-668-3701, jennifer@cwcomm.org
 
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